Objective To evaluate the effects of mitochondrial ATP-sensitive potassium channel opener diazoxide on ultrastructural changes in myocardial cells and myocyte mortality in isoproterenol-induced myocardial ischemic rats. Methods Thirty Wistar rats were randomly divided into 3 groups: control group, myocardial ischemic group (with 5 mg/kg isoproterenol injection subcutaneously) and experimental group (20 mg/kg diazoxide injection before the ischemic injure). Results Isoproterenol injection could damage the myocardial cell ultrastructures, which could be mitigated by preconditioning diazoxide injection. 10-100 μmol/l diazoxide could significantly decrease the mortality of ischemic myocardial cells compared to the control group (P0.01). Conclusions Mitochondrial ATP-sensitive potassium channel opener diazoxide has a cardioprotective effect on myocardial ischemia.